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Assay Detail

CHEMBL757380

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of Mu opioid receptor of mouse vas deferens
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Mu-type opioid receptor (CHEMBL2858)
Type SINGLE PROTEIN
Organism Mus musculus

Publication

Structure-activity study on the Phe side chain arrangement of endomorphins using conformationally constrained analogues.
Tömböly C, Kövér KE, Péter A, Tourwé D, Biyashev D, Benyhe S, Borsodi A, Al-Khrasani M, Rónai AZ, Tóth G.
J Med Chem (2004) 47 : 735 -743
PubMed 14736254 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.43 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL436039 1 8.04
CHEMBL333357 ENDOMORPHIN 2 1 7.62
CHEMBL316446 ENDOMORPHIN-1 1 7.44
CHEMBL163334 1 6.63
CHEMBL349738 1 -
CHEMBL355141 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL436039 IC50 = 9.15 nM 8.04
CHEMBL333357 ENDOMORPHIN 2 IC50 = 24.1 nM 7.62
CHEMBL316446 ENDOMORPHIN-1 IC50 = 36.3 nM 7.44
CHEMBL163334 IC50 = 235.0 nM 6.63
CHEMBL349738 IC50 > 10000.0 nM -
CHEMBL355141 IC50 > 10000.0 nM -